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GPCRs

 

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Application note: NanoBRETTM assay for monitoring of ligand binding to GPCRs in live cells, using the CLARIOstar® and the PHERAstar® FS

17 September 2018 | By

Due to the crucial role of G protein-coupled receptors (GPCRs) in mediating cellular responses to external stimuli, these receptors have been and will remain a prime focus for medical research and the pharmaceutical industry for many years to come. Their importance is especially highlighted by the statistic that 30-50% of…

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Expert view: Managing the complexity of finding new targets and drugging the undruggable

5 September 2018 | By

Assessing targets that are unable – or rather, extremely difficult – to reach pharmacologically, has prevented researchers from achieving desired clinical successes, most notably in the realm of cancer research. However, many advances are being made to shedlight on these difficult yet desirable target areas.

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High-throughput calcium flux assays: luminescent versus fluorescent readout

20 September 2016 | By , , ,

In vitro high-throughput cellular target-based assays are commonly used for hit identification targeting G-protein coupled receptors (GPCR). Agonist and antagonist identification of GPCRs often relies on the screening of large collections of chemicals using miniaturised in vitro cell-based functional assays. In the panel of assays, calcium mobilisation measured by aequorin…